LY3200882

Cas No.:	1898283-02-7
Chemical Name:	2-(4-((4-((1-Cyclopropyl-3-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl)oxy)pyridin-2-yl)amino)pyridin-2-yl)propan-2-ol
Synonyms:	LY3200882;19HY34R6UN;2-(4-((4-((1-cyclopropyl-3-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl)oxy)pyridin-2-yl)amino)pyridin-2-yl)propan-2-ol;2-{4-[(4-{[1-cyclopropyl-3-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl]oxy}pyridin-2-yl)amino]pyridin-2-yl}propan-2-ol;LY 3200882;BCP20882;s8772;A16816;C1(CC1)N1N=C(C(=C1)OC1=CC(=NC=C1)NC1=CC(=NC=C1)C(C)(C)O)C1CCOCC1;2-[4-[[4-[1-Cyclopropyl-3-(oxan-4-yl)pyrazol-4-yl]
SMILES:	O1C([H])([H])C([H])([H])C([H])(C([H])([H])C1([H])[H])C1C(=C([H])N(C2([H])C([H])([H])C2([H])[H])N=1)OC1C([H])=C([H])N=C(C=1[H])N([H])C1C([H])=C([H])N=C(C=1[H])C(C([H])([H])[H])(C([H])([H])[H])O[H]
Formula:	C24N5O3H29
M.Wt:	435.5188
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	LY3200882 is a novel and highly selective inhibitor of TGF-β receptor type 1 (TGFβRI).
Target:	TGFβRI[1]
In Vivo:	LY3200882 potently inhibits TGFβ mediated SMAD phosphorylation in vivo in subcutaneous tumors in a dose dependent fashion. LY3200882 has shown anti-metastatic activity in vivo in an experimental metastasis tumor model (intravenous EMT6-LM2 model of triple negative breast cancer)[1].
In Vitro:	LY3200882 is a novel, highly selective inhibitor of TGF-β receptor type 1 (TGFβRI). LY3200882 potently inhibits TGFβ mediated SMAD phosphorylation in vitro in tumor and immune cells. LY3200882 has shown anti-metastatic activity in vitro in migration assays. In in vitro immune suppression assays, LY3200882 has shown the ability to rescue TGFβ1 suppressed or T regulatory cell suppressed naïve T cell activity and restore proliferation[1].
References:	[1]. Huaxing Pei, et al. Abstract 955: LY3200882, a novel, highly selective TGFβRI small molecule inhibitor. AACR; Cancer Res 2017;77(13 Suppl):Abstract nr 955.